A multi-kinase inhibitor
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Active Metabolite(s)
35102N-desmethyl Regorafenib N-oxide
Labeled Version(s)
25486Regorafenib-13C-d3
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Regorafenib

Item No. 18498

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide
CAS Number
755037-03-7
Synonyms
  • BAY 73-4506
Molecular Formula
C21H15ClF4N4O3
Formula Weight
482.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 30 mg/mlEthanol: 14 mg/ml
λmax
263 nm
SMILES
O=C(NC)C1=CC(OC2=CC=C(NC(NC3=CC(C(F)(F)F)=C(Cl)C=C3)=O)C(F)=C2)=CC=N1
InChi Code
InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
InChi Key
FNHKPVJBJVTLMP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity.1 It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectivey) as well as other kinases.1,2,3 In vivo, regorafenib (10 mg/kg) reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models.1 It also reduces tumor microvessel area and inhibits tumor growth in a panel of mouse xenograft models. Formulations containing regorafenib have been used in the treatment of advanced gastrointestinal stromal tumors and metastatic colorectal cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wilhelm, S.M., Dumas, J., Adnane, L., et al. Regorafenib (BAY 73-4506): A new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int. J. Cancer 129(1), 245-255 (2011).

    2. Uitdehaag, J.C.M., de Roos, J.A.D.M., van Doornmalen, A.M., et al. Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use. PLoS One 9(3), 1-13 (2014).

    3. Ravi, S., and Singal, A.K. Regorafenib: An evidence-based review of its potential in patients with advanced liver cancer. Core Evid. 9, 81-87 (2014).